Id: acc0172
Group: 1sens
Protein: Src
Gene Symbol: SRC
Protein Id: P12931
Protein Name: SRC_HUMAN
PTM: phosphorylation
Site: Tyr419
Site Sequence: LARLIEDNEYTARQGAKFPIK
Disease Category: Cancer
Disease: Sarcoma
Disease Subtype: osteosarcoma
Disease Cellline: 143B?
Disease Info:
Drug: dasatinib
Drug Info: "Dasatinib is a tyrosine kinase inhibitor that targets BCR-ABL and SRC family kinases, used in the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), particularly in patients resistant or intolerant to prior therapy including imatinib."
Effect: modulate
Effect Info: "In vitro, the drug inhibits osteosarcoma by suppressing Src phosphorylation."
Note:
Score: 4.0
Pubmed(PMID): 19447875
Sentence Index:
Sentence:

Sequence & Structure:

MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAEPKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGDWWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRESETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGLCHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
SRC DASATINIB SRC inhibitor 4 - acute lymphoblastic leukemia DailyMed
DailyMed
SRC DASATINIB SRC inhibitor 4 Unknown status acute lymphoblastic leukemia ClinicalTrials
SRC DASATINIB SRC inhibitor 4 - chronic myelogenous leukemia DailyMed
DailyMed
SRC DASATINIB SRC inhibitor 4 Completed chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
SRC DASATINIB SRC inhibitor 4 Unknown status chronic myelogenous leukemia ClinicalTrials
SRC DASATINIB SRC inhibitor 4 Recruiting chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
ClinicalTrials
SRC VANDETANIB Tyrosine-protein kinase SRC inhibitor 4 - neoplasm ATC
SRC DASATINIB SRC inhibitor 4 - neoplasm ATC
SRC TIRBANIBULIN Tyrosine-protein kinase SRC inhibitor 4 Completed actinic keratosis ClinicalTrials
ClinicalTrials
SRC TIRBANIBULIN Tyrosine-protein kinase SRC inhibitor 4 Recruiting actinic keratosis ClinicalTrials
SRC TIRBANIBULIN Tyrosine-protein kinase SRC inhibitor 4 - actinic keratosis FDA
DailyMed
EMA
SRC TIRBANIBULIN Tyrosine-protein kinase SRC inhibitor 4 Withdrawn actinic keratosis ClinicalTrials
SRC VANDETANIB Tyrosine-protein kinase SRC inhibitor 4 - thyroid carcinoma DailyMed
SRC VANDETANIB Tyrosine-protein kinase SRC inhibitor 4 - thyroid neoplasm EMA
SRC DASATINIB SRC inhibitor 4 - lymphoid leukemia EMA
SRC DASATINIB SRC inhibitor 4 - Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive EMA
SRC VANDETANIB Tyrosine-protein kinase SRC inhibitor 4 Active, not recruiting thyroid cancer ClinicalTrials
SRC VANDETANIB Tyrosine-protein kinase SRC inhibitor 4 - medullary thyroid gland carcinoma DailyMed
SRC DASATINIB SRC inhibitor 3 Active, not recruiting acute lymphoblastic leukemia ClinicalTrials
SRC DASATINIB SRC inhibitor 3 Not yet recruiting acute lymphoblastic leukemia ClinicalTrials
SRC DASATINIB SRC inhibitor 3 Completed acute lymphoblastic leukemia ClinicalTrials
ClinicalTrials
SRC DASATINIB SRC inhibitor 3 Completed acute myeloid leukemia ClinicalTrials
SRC BOSUTINIB Tyrosine-protein kinase SRC inhibitor 3 Active, not recruiting chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
SRC BOSUTINIB Tyrosine-protein kinase SRC inhibitor 3 Completed chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
SRC BOSUTINIB Tyrosine-protein kinase SRC inhibitor 3 Not yet recruiting chronic myelogenous leukemia ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
SRC-Tyr419
Cancer Intensity
BRCA
COAD -0.413
HGSC 1.82
ccRCC -0.985
GBM
HNSC -0.869
LUAD
LUSC 0.833
non_ccRCC
PDAC -0.088
UCEC -0.297

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 419 D Barrett's neoplasia Phosphorylation 14608530
Y 419 D Oral squamous cell carcinoma Phosphorylation 23707351
Y 419 P Acute myeloid leukemia/acute myelogenous leukemia Phosphorylation 18056483
Y 419 U Breast cancer Phosphorylation 17967179
Y 419 U Breast cancer/tumor/carcinoma Phosphorylation 24358106 ;  26923594 ;  21490376 ;  17967179
Y 419 U Colon cancer/carcinoma Phosphorylation 17148760
Y 419 U Glioma/adult gliomas Phosphorylation 24358106
Y 419 U Ovarian cancer Phosphorylation 32294438
Y 419 U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 17045208
Y 419 U Triple-negative breast cancer Phosphorylation 26923594
Y 419 U Gestational choriocarcinoma Phosphorylation 23671128
Y 419 U Glioblastoma Phosphorylation 22323579
Y 419 U Triple-negative breast cancer Phosphorylation 26923594

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: